1. Protein Tyrosine Kinase/RTK
    JAK/STAT Signaling
  2. EGFR
  3. PKI-166 hydrochloride

PKI-166 hydrochloride 

Cat. No.: HY-110328
Handling Instructions

PKI-166 hydrochloride is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM.

For research use only. We do not sell to patients.

PKI-166 hydrochloride Chemical Structure

PKI-166 hydrochloride Chemical Structure

CAS No. : 2230253-82-2

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Description

PKI-166 hydrochloride is a potent, selective and orally bioavailable EGFR tyrosine kinase inhibitor, with an IC50 of 0.7 nM[1].

IC50 & Target

IC50: 0.7 nM (EGFR tyrosine kinase)[1]

In Vitro

Pretreatment with PKI-166 hydrochloride (0-0.5 μM; 1 hour) inhibits EGFR autophosphorylation in human pancreatic cancer cells[1].
PKI-166 hydrochloride (0.03 μM; 6 days) enhances the cytotoxicity mediated by gemcitabine[1].

Western Blot Analysis[1]

Cell Line: L3.6pl cells
Concentration: 0.01 μM, 0.05 μM, 0.5 μM
Incubation Time: 1 hour
Result: Inhibited EGFR autophosphorylation in a dose-dependent manner.

Cell Cytotoxicity Assay[1]

Cell Line: L3.6pl cells
Concentration: 0.03 μM
Incubation Time: 6 days
Result: Enhanced the cytotoxicity mediated by gemcitabine.
In Vivo

PKI-166 hydrochloride (100 mg/kg; p.o.; daily; day 7-day 35 after xenograft) inhibits of pancreatic cancer growth[1].

Animal Model: Male athymic nude mice with L3.6pl cells xenograft (8–12 weeks)[1]
Dosage: 100 mg/kg
Administration: Oral administration; daily; from day 7 to day 35 after xenograft
Result: Significantly decreased median tumor volume.
Molecular Weight

366.84

Formula

C₂₀H₁₉ClN₄O

CAS No.

2230253-82-2

SMILES

OC1=CC=C(C2=CC3=C(N=CN=C3N2)N[[email protected]](C)C4=CC=CC=C4)C=C1.Cl[H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PKI-166PKI166PKI 166EGFREpidermal growth factor receptorErbB-1HER1tyrosinekinase,EGFR-TKIpancreaticcancerInhibitorinhibitorinhibit

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PKI-166 hydrochloride
Cat. No.:
HY-110328
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